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Osmotic pump tablet capable of loading large-dose slightly-soluble medicaments and promoting absorption thereof

A technology of insoluble drugs and osmotic pumps, which is applied in the field of medicine and can solve the problem of reducing the loading of drugs

Inactive Publication Date: 2013-06-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the increase in the amount of such compounds will make the amount of drug loading relatively reduced

Method used

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  • Osmotic pump tablet capable of loading large-dose slightly-soluble medicaments and promoting absorption thereof
  • Osmotic pump tablet capable of loading large-dose slightly-soluble medicaments and promoting absorption thereof
  • Osmotic pump tablet capable of loading large-dose slightly-soluble medicaments and promoting absorption thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]

[0036] Tablet preparation:

[0037] Pass the original and auxiliary materials through a 100-mesh sieve respectively, weigh the prescribed amount of sildenafil citrate, fully mix them with sorbitol, hydroxypropyl cellulose, and hydroxyethyl cellulose, and then add the prescribed amount of magnesium stearate and mix evenly. A tablet press presses tablets to obtain tablet cores.

[0038] Coating Solution Prescription:

[0039] Cellulose acetate 66.7%

[0040] Macrogol 4000 33.3%

[0041] Coating process:

[0042] Dissolve the semipermeable membrane coating material and the plasticizer porogen in the mixed solvent of acetone-water, place the tablet core in a coating pan for coating, and the coating process is as follows: the flow rate of the coating solution is 2.5ml / min, The temperature in the coating pan is 30°C, and the rotation speed is 8-10rpm. After the weight gain of the coating reaches 8%-12%, the coated tablet is dried in an oven at 36° C. for 12 hours. ...

Embodiment 2

[0045]

[0046] Tablet preparation:

[0047]Pass the original and auxiliary materials through a 100-mesh sieve respectively, weigh the prescribed amount of Glichet, mix well with sodium chloride, hydroxypropyl cellulose, and hydroxyethyl cellulose, and then add the prescribed amount of magnesium stearate and mix evenly. A tablet press presses tablets to obtain tablet cores.

[0048] Coating Solution Prescription:

[0049] Cellulose acetate 66.7%

[0050] Macrogol 4000 33.3%

[0051] Coating process:

[0052] Dissolve the semipermeable membrane coating material and the plasticizer porogen in the mixed solvent of acetone-water, place the tablet core in a coating pan for coating, and the coating process is as follows: the flow rate of the coating solution is 2.5ml / min, The temperature in the coating pan is 30°C, and the rotation speed is 8-10rpm. After the weight gain of the coating reaches 8%-12%, the coated tablet is dried in an oven at 36° C. for 12 hours. The dried c...

Embodiment 3

[0055]

[0056] Tablet preparation:

[0057] Pass the original and auxiliary materials through a 100-mesh sieve, weigh the prescribed amount of G004, mix well with sodium chloride, hydroxypropyl cellulose, and hydroxyethyl cellulose, and then add the prescribed amount of talcum powder and mix well. A tablet press presses tablets to obtain tablet cores.

[0058] Coating Solution Prescription:

[0059] Cellulose acetate 83.3%

[0060] Macrogol 4000 16.7%

[0061] Coating process: dissolve the semipermeable membrane coating material and plasticizer porogen in the mixed solvent of acetone-water, and place the tablet core in the coating pan for coating. The coating process is as follows: the flow rate of the coating solution is 2.5 ml / min, the temperature inside the coating pan is 30°C, and the rotation speed is 8-10rpm. After the weight gain of the coating reaches 8%-12%, the

[0062] The coated tablets were dried in an oven at 36°C for 12 hours. The dried coated tablet i...

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PUM

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Abstract

The invention provides an osmotic pump tablet capable of loading large-dose slightly-soluble medicaments and promoting absorption thereof. The preparation tablet core is a single layer tablet, including a medicament, an absorption promoting agent, a penetration enhancer, an absorbent, a disintegrating agent, an adhesive polymer and lubricant, wherein the medicament is dissolved in the absorption promoting agent, uniformly mixed with the penetration enhancer, the absorbent, the disintegrating agent and the adhesive polymer, and is granulated; and the lubricant is added after the mixture is baked, and the mixture is tabletted to obtain the tablet core. A coating film is coated outside the tablet core, and a pore is formed on any side of the coating film. The adhesive polymer is hydroxyethylcellulose, which can disperse the medicament uniformly when the dose of the hydroxyethyl cellulose in the prescription is 3 percent, and the medicament is released durably and stably, so that the aimof loading slightly-soluble medicaments in the osmotic pump tablets in large dose is realized. The absorption effect of the slightly-soluble medicaments is remarkably improved by adding the absorption promoting agent. The medicine content of the preparation can be 500mg, so that the medicament is controlled to release in a constant speed, the drug action is durable and stable, the number of administration is small, and the toxic and side effects are slight. The osmotic pump tablet has the advantages of more in-vivo absorption, high bioavailability and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an osmotic pump tablet capable of loading a large dose of insoluble drug and promoting its absorption and a preparation method thereof. Background technique [0002] According to statistics, water-insoluble drugs account for about 40% of the world's total drugs, and there are large differences in drug absorption within and between individuals. Existing common problems have caused great difficulties to their development and utilization. [0003] For insoluble drugs, it is difficult to make them into osmotic pump tablets, because of their low solubility (Cs), it is difficult to form a higher concentration and osmotic pressure in the microenvironment of the tablet core to maintain an effective drug release rate, or to To maintain a long-lasting and constant osmotic pressure requires a large amount of osmotic pressure enhancer (beyond the normal tablet weight range), so insoluble d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/44A61K47/38A61K47/32A61K9/30
Inventor 葛亮陈艳华田野朱家壁刘建平
Owner CHINA PHARM UNIV